Tamsulosin

Last updated

Tamsulosin
Tamsulosin.svg
Tamsulosin-from-xtal-3D-bs-17.png
Clinical data
Pronunciation /tæmˈsuːləsɪn/ [1]
tam-SOO-lə-sin
Trade names Flomax, others
AHFS/Drugs.com Monograph
MedlinePlus a698012
License data
Pregnancy
category
  • AU:B2
Routes of
administration 		By mouth
ATC code
Legal status
Legal status
Pharmacokinetic data
Bioavailability 100% (by mouth)
Metabolism Liver
Elimination half-life 9–13 hours
Excretion 76% Kidney
Identifiers
  • (R)-5-(2-{[2-(2-Ethoxyphenoxy)ethyl]amino}propyl)-2-methoxybenzene-1-sulfonamide
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard (EPA)
ECHA InfoCard 100.109.780 OOjs UI icon edit-ltr-progressive.svg
Chemical and physical data
Formula C20H28N2O5S
Molar mass 408.51 g·mol−1
3D model (JSmol)
  • CCOc1ccccc1OCCN[C@@H](C)Cc1ccc(OC)c(c1)S(=O)(=O)N
  • InChI=1S/C20H28N2O5S/c1-4-26-17-7-5-6-8-18(17)27-12-11-22-15(2)13-16-9-10-19(25-3)20(14-16)28(21,23)24/h5-10,14-15,22H,4,11-13H2,1-3H3,(H2,21,23,24)/t15-/m1/s1 Yes check.svgY
  • Key:DRHKJLXJIQTDTD-OAHLLOKOSA-N Yes check.svgY
   (verify)
Tamsulosin - ARISTO Pharma - 0.4 mg prolonged-release tablets - Urologikum Tamsulosin - ARISTO Pharma - 0,4 mg Retardtabletten - Urologikum.jpg
Tamsulosin – ARISTO Pharma – 0.4 mg prolonged-release tablets – Urologikum

Tamsulosin, sold under the brand name Flomax among others, is a medication used to treat symptomatic benign prostatic hyperplasia (BPH) and chronic prostatitis and to help with the passage of kidney stones. [6] [7] [8] The evidence for benefit with a kidney stone is better when the stone is larger. [8] Tamsulosin is taken by mouth. [6]

Contents

Common side effects include dizziness, headache, sleeplessness, nausea, blurry vision, and sexual problems. [9] [6] Other side effects may include feeling lightheaded with standing due to changes in blood pressure, and angioedema. [9] Tamsulosin is an alpha blocker and works by relaxing muscles in the prostate. [10] Specifically it is an α1 adrenergic receptor blocker. [6]

Tamsulosin was approved for medical use in the United States in 1997. [6] It is available as a generic medication. [9] In 2021, it was the 24th most commonly prescribed medication in the United States, with more than 23 million prescriptions. [11] [12]

Medical uses

Flomax 0.4 mg oral capsule 000636lg Flomax 0.4 mg.jpg
Flomax 0.4 mg oral capsule

Tamsulosin is primarily used for benign prostatic hyperplasia (BPH) and to help with the passage of kidney stones. [13] [14] Tamsulosin, however, appears to be effective only for stones over 4 mm and less than 10 mm in size. [8]

Tamsulosin is also used as an add-on treatment for acute urinary retention. People may void more successfully after catheter removal if they are taking tamsulosin. People taking tamsulosin also are less likely to need recatheterization. [15]

Tamsulosin does not decrease the overall size of the prostate in men with BPH, and is not recommended for prevention of prostate cancer. [16]

Combination therapy

The results of the CombAT (combination of dutasteride (Avodart) and tamsulosin, under the brand name Duodart) trial in 2008 demonstrated that treatment with the combination of dutasteride and tamsulosin provides greater symptom benefits compared to monotherapy with either agent alone for treatment of benign prostatic hyperplasia. [17] The CombAT trial became the medication Jalyn. It was approved by the FDA on 14 June 2010. [18] This combination can be useful because it may take up to six months for symptomatic relief to be found when using 5-alpha-reductase inhibitors such as dutasteride compared to alpha-1 receptor blockers, which can provide relief in some cases within 48 hours. [19]

Adverse effects

Mechanism

Tamsulosin is a selective α1 receptor antagonist that has preferential selectivity for the α1A receptor in the prostate versus the α1B receptor in the blood vessels. [25]

When alpha 1 receptors in the bladder neck, prostate, ureter, and urethra are blocked, a relaxation in smooth muscle tissue results. [16] This mechanism decreases resistance to urinary flow, reduces discomfort associated with BPH, and facilitates passage of kidney stones. [16]

Brand names

Tamsulosin was first marketed in 1996 under the trade name Flomax. The U.S. patent expired in October 2009. [26] The U.S. Food and Drug Administration (FDA) approved generics in March 2010. [27] In 2010, tamsulosin was available as OTC medication in UK. [28]

It is marketed by various companies under licence, including Boehringer Ingelheim and CSL. Tamsulosin hydrochloride extended-release capsules are marketed under the trade names Urimax 0.4 (India),Tamlocept 0.4 (India), Flomax, Flomaxtra, Contiflo XL, bestflo, Mecir LP (France), Urimax, Pamsvax, and Pradif, [29] although generic, unmodified-release capsules are still approved and marketed in many countries (such as Canada). Generic extended-release tablets are marketed in most countries of the EEA. [30] In Mexico, it is marketed as Secotex and as Harnal D in Japan and Indonesia and as Harnal OCAS (oral controlled absorption system) in Thailand. [31] In Egypt, [32] Italy, Russia and Iceland, it is marketed under the trade name Omnic by Astellas Pharma Europe. The largest manufacturer of tamsulosin is Synthon BV (the Netherlands).[ citation needed ] Tamsulosin hydrochloride is marketed in Bangladesh under the trade names Uromax, Prostanil MR, Tamisol MR, and Tamsin.[ citation needed ]

Related Research Articles

<span class="mw-page-title-main">Benign prostatic hyperplasia</span> Noncancerous increase in size of the prostate gland

Benign prostatic hyperplasia (BPH), also called prostate enlargement, is a noncancerous increase in size of the prostate gland. Symptoms may include frequent urination, trouble starting to urinate, weak stream, inability to urinate, or loss of bladder control. Complications can include urinary tract infections, bladder stones, and chronic kidney problems.

<span class="mw-page-title-main">Tadalafil</span> Medication used to treat erectile dysfunction

Tadalafil, sold under the brand name Cialis among others, is a medication used to treat erectile dysfunction, benign prostatic hyperplasia, and pulmonary arterial hypertension. It is taken by mouth. Onset is typically within half an hour and the duration is up to 36 hours.

<span class="mw-page-title-main">Vardenafil</span> Chemical compound

Vardenafil, sold under the brand name Levitra among others, is a medication that is used for treating erectile dysfunction. It is a PDE5 inhibitor. It is taken by mouth.

<span class="mw-page-title-main">Urinary retention</span> Inability to completely empty the bladder

Urinary retention is an inability to completely empty the bladder. Onset can be sudden or gradual. When of sudden onset, symptoms include an inability to urinate and lower abdominal pain. When of gradual onset, symptoms may include loss of bladder control, mild lower abdominal pain, and a weak urine stream. Those with long-term problems are at risk of urinary tract infections.

<span class="mw-page-title-main">Finasteride</span> Antiandrogen medication

Finasteride, sold under the brand names Proscar and Propecia among others, is a medication used to treat pattern hair loss and benign prostatic hyperplasia (BPH) in men. It can also be used to treat excessive hair growth in women. It is usually taken orally but there are topical formulations for patients with hair loss, designed to minimize systemic exposure by acting specifically on hair follicles.

<span class="mw-page-title-main">5α-Reductase inhibitor</span> Class of medications

5α-Reductase inhibitors (5-ARIs), also known as dihydrotestosterone (DHT) blockers, are a class of medications with antiandrogenic effects which are used primarily in the treatment of enlarged prostate and scalp hair loss. They are also sometimes used to treat excess hair growth in women and as a component of hormone therapy for transgender women.

<span class="mw-page-title-main">Doxazosin</span> Group of stereoisomers

Doxazosin, sold under the brand names Cardura among others, is a medication used to treat symptoms of benign prostatic hyperplasia and hypertension. For high blood pressure, it is a less preferred option. It is taken by mouth.

<span class="mw-page-title-main">Dutasteride</span> Hormone replacement medication

Dutasteride, sold under the brand name Avodart among others, is a medication primarily used to treat the symptoms of a benign prostatic hyperplasia (BPH), an enlarged prostate not associated with cancer. A few months may be required before benefits occur. It is also used for scalp hair loss in men and as a part of hormone therapy in transgender women. It is usually taken by mouth.

<span class="mw-page-title-main">Prazosin</span> Antihypertensive drug

Prazosin, sold under the brand name Minipress among others, is a medication used to treat high blood pressure, symptoms of an enlarged prostate, and nightmares related to post-traumatic stress disorder (PTSD). It is an α1 blocker. It is a less preferred treatment of high blood pressure. Other uses may include heart failure and Raynaud syndrome. It is taken by mouth.

<span class="mw-page-title-main">Alfuzosin</span> Chemical compound alfa1-blocker

Alfuzosin, sold under the brand name Uroxatral among others, is a medication of the α1 blocker class. It is used to treat benign prostatic hyperplasia (BPH).

Alpha-1 blockers constitute a variety of drugs that block the effect of catecholamines on alpha-1-adrenergic receptors. They are mainly used to treat benign prostatic hyperplasia (BPH), hypertension and post-traumatic stress disorder. Alpha-1 adrenergic receptors are present in vascular smooth muscle, the central nervous system, and other tissues. When alpha blockers bind to these receptors in vascular smooth muscle, they cause vasodilation.

Nocturia is defined by the International Continence Society (ICS) as "the complaint that the individual has to wake at night one or more times for voiding ". The term is derived from Latin nox – "night", and Greek [τα] ούρα – "urine". Causes are varied and can be difficult to discern. Although not every patient needs treatment, most people seek treatment for severe nocturia, waking up to void more than 2–3 times per night.

Intraoperative floppy iris syndrome (IFIS) is a complication that may occur during cataract extraction in certain patients. This syndrome is characterized by a flaccid iris which billows in response to ordinary intraocular fluid currents, a propensity for this floppy iris to prolapse towards the area of cataract extraction during surgery, and progressive intraoperative pupil constriction despite standard procedures to prevent this.

<span class="mw-page-title-main">Silodosin</span> Chemical compound

Silodosin, sold under the brand name Urief among others, is a medication for the symptomatic treatment of benign prostatic hyperplasia. It acts as an alpha-1 adrenergic receptor antagonist.

Lower urinary tract symptoms (LUTS) refer to a group of clinical symptoms involving the bladder, urinary sphincter, urethra and, in men, the prostate. The term is more commonly applied to men – over 40% of older men are affected – but lower urinary tract symptoms also affect women. The condition is also termed prostatism in men, but LUTS is preferred.

<span class="mw-page-title-main">Alpha blocker</span> Class of pharmacological agents

Alpha-blockers, also known as α-blockers or α-adrenoreceptor antagonists, are a class of pharmacological agents that act as antagonists on α-adrenergic receptors (α-adrenoceptors).

<span class="mw-page-title-main">Epristeride</span> Chemical compound

Epristeride, sold under the brand names Aipuliete and Chuanliu, is a medication which is used in the treatment of enlarged prostate in China. It is taken by mouth.

Dutasteride/tamsulosin, sold under the brand name Jalyn among others, is a medication produced by GlaxoSmithKline for the treatment of adult male symptomatic benign prostatic hyperplasia (BPH). It is a combination of two previously existing medications: dutasteride, brand name Avodart, and tamsulosin, brand name Flomax. It contains 0.5 mg of dutasteride and 0.4 mg of tamsulosin hydrochloride.

Adrenergic blocking agents are a class of drugs that exhibit its pharmacological action through inhibiting the action of the sympathetic nervous system in the body. The sympathetic nervous system(SNS) is an autonomic nervous system that we cannot control by will. It triggers a series of responses after the body releases chemicals named noradrenaline and epinephrine. These chemicals will act on adrenergic receptors, with subtypes Alpha-1, Alpha-2, Beta-1, Beta-2, Beta-3, which ultimately allow the body to trigger a "fight-or-flight" response to handle external stress. These responses include vessel constriction in general vessels whereas there is vasodilation in vessels that supply skeletal muscles or in coronary vessels. Additionally, the heart rate and contractile force increase when SNS is activated, which may be harmful to cardiac function as it increases metabolic demand.

Finasteride/tadalafil, sold under the brand name Entadfi, is a fixed-dose combination medication used for the treatment of benign prostatic hyperplasia (BPH). It contains finasteride and tadalafil. It is taken by mouth.

References

  1. ↑ "Tamsulosin". Merriam-Webster.com Dictionary .
  2. ↑ "Product monograph brand safety updates". Health Canada. February 2024. Retrieved 24 March 2024.
  3. ↑ "Flomaxtra XL, 400 micrograms, film-coated prolonged release tablet – Summary of Product Characteristics (SmPC)". (emc). 12 November 2019. Retrieved 2 December 2021.
  4. ↑ "Faramsil 400 microgram Prolonged-release Tablets – Summary of Product Characteristics (SmPC)". (emc). 4 November 2020. Retrieved 2 December 2021.
  5. ↑ "Flomax– tamsulosin hydrochloride capsule". DailyMed. Retrieved 2 December 2021.
  6. 1 2 3 4 5 "Tamsulosin Hydrochloride Monograph for Professionals". Drugs.com. AHFS. Retrieved 24 December 2018.
  7. ↑ "Prostatitis". NHS. 19 October 2017. Retrieved 24 December 2018.
  8. 1 2 3 Wang RC, Smith-Bindman R, Whitaker E, Neilson J, Allen IE, Stoller ML, Fahimi J (March 2017). "Effect of Tamsulosin on Stone Passage for Ureteral Stones: A Systematic Review and Meta-analysis". Annals of Emergency Medicine. 69 (3): 353–361.e3. doi: 10.1016/j.annemergmed.2016.06.044 . PMID   27616037.
  9. 1 2 3 British national formulary : BNF 76 (76 ed.). Pharmaceutical Press. 2018. p. 767. ISBN   9780857113382.
  10. ↑ Hutchison LC, Sleeper RB (2010). Fundamentals of Geriatric Pharmacotherapy: An Evidence-Based Approach. ASHP. p. 209. ISBN   9781585283057.
  11. ↑ "The Top 300 of 2021". ClinCalc. Archived from the original on 15 January 2024. Retrieved 14 January 2024.
  12. ↑ "Tamsulosin –Drug Usage Statistics". ClinCalc. Retrieved 14 January 2024.
  13. ↑ "Tamsulosin Aids Stone Expulsion". Renal and Urology News. 7 January 2011.
  14. ↑ "Study Shows Use of Tamsulosin or Nifedipine Helps Patients to Clear Ureteral Stone Fragments Faster and Reduces Rate of Recurrence".
  15. ↑ Lucas MG, Stephenson TP, Nargund V (February 2005). "Tamsulosin in the management of patients in acute urinary retention from benign prostatic hyperplasia". BJU International. 95 (3): 354–357. doi:10.1111/j.1464-410X.2005.05299.x. PMID   15679793. S2CID   30254915.
  16. 1 2 3 Lewis SM, Dirksen SR, Heitkemper MM, Bucher LH (2013). Medical-surgical nursing : assessment and management of clinical problems (9th ed.). St. Louis, Missouri. ISBN   978-0-323-10089-2. OCLC   228373703.{{cite book}}: CS1 maint: location missing publisher (link)
  17. ↑ Roehrborn CG, Siami P, Barkin J, Damião R, Major-Walker K, Morrill B, Montorsi F (February 2008). "The effects of dutasteride, tamsulosin and combination therapy on lower urinary tract symptoms in men with benign prostatic hyperplasia and prostatic enlargement: 2-year results from the CombAT study". The Journal of Urology. 179 (2): 616–621, discussion 621. doi:10.1016/j.juro.2007.09.084. PMID   18082216.
  18. ↑ FDA approval letter at FDA.gov
  19. ↑ Australian Medicines Handbook [ full citation needed ]
  20. ↑ Medscape, Good Cataract Surgery Outcomes Possible in Intraoperative Floppy Iris Syndrome Due to Tamsulosin.
  21. ↑ Bird ST, Delaney JA, Brophy JM, Etminan M, Skeldon SC, Hartzema AG (November 2013). "Tamsulosin treatment for benign prostatic hyperplasia and risk of severe hypotension in men aged 40-85 years in the United States: risk window analyses using between and within patient methodology". BMJ. 347: f6320. doi:10.1136/bmj.f6320. PMC   3817852 . PMID   24192967.
  22. ↑ Ramirez J (November 2013). "Severe hypotension associated with α blocker tamsulosin". BMJ. 347: f6492. doi:10.1136/bmj.f6492. hdl: 10906/78488 . PMID   24192968. S2CID   24324483.
  23. ↑ Page RL, O'Bryant CL, Cheng D, Dow TJ, Ky B, Stein CM, et al. (August 2016). "Drugs That May Cause or Exacerbate Heart Failure: A Scientific Statement From the American Heart Association". Circulation. 134 (6): e32–e69. doi: 10.1161/CIR.0000000000000426 . PMID   27400984.
  24. ↑ "Tamsulosin Side Effects". Drugs.com. Retrieved 27 April 2011.
  25. ↑ Shen H (2008). Illustrated Pharmacology Memory Cards: PharMnemonics. Minireview. p. 13. ISBN   978-1-59541-101-3.
  26. ↑ "Flomax – Big Patent Expirations of 2010". 10 February 2010. Archived from the original on 22 April 2012. Retrieved 14 January 2012.
  27. ↑ "FDA Approves First Generic Tamsulosin to Treat Enlarged Prostate Gland" (Press release). U.S. Food and Drug Administration (FDA). 2 March 2010.
  28. ↑ "OTC tamsulosin for benign prostatic hyperplasia". Drug and Therapeutics Bulletin. 48 (10): 113–116. October 2010. doi:10.1136/dtb.2010.10.0052. PMID   20926447. S2CID   32141889.
  29. ↑ Magnanelli S, Vetere AM. "Pradif 0,4 Mg Capsule Rigide A Rilascio Prolungato". Torrinomedica.it. Retrieved 15 November 2012.
  30. ↑ "Tamsulosina Mylan 0,4 mg cápsulas duras de liberación modificada EFG" (PDF). cima.aemps.es. Retrieved 29 October 2018.
  31. ↑ "Drugs.com Database".
  32. ↑ "Novartis hits Astellas with transplant drug generic". Reuters. 11 August 2009. Retrieved 11 August 2009.
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